r
`--------···--· ---------
`\.
`-------~--- -·-·-- ·- --~---
`
`EDITION
`
`1996
`
`PHYSCANS'
`DESK
`REFERENCE®
`
`Medical Consultant
`Ronald Arky, MD, Charles S. Davidson Professor of Medicine and Master, Francis Weld Peabody Society, Harvard Medical School
`
`President and Chief Operating Officer, Drug Information Services Group: Thomas F. Rice
`Vice President of Production: Steven R. Andreazza
`Director of Product Management: Stephen B. Greenberg
`Associate Product Managers: Cy s. Caine, Howard N. Kanter
`Manager, Database Administration: Lynne Handler
`Contracts and Support Services Director: Marjorie A. Duffy
`National Sales Manager: James R. Pantaleo
`Senior Account Manager: Michael s. Sarajian
`Director of Production: Carrie Williams
`Production Managers: Kimberly Hiller-Vivas, Tara L. Walsh
`Account Managers
`Production Coordinators: Amy B. Douma, Dawn B. McCall
`Dikran N. Barsamian
`Donald V. Bruccoleri
`Format Editors: Gregory J. Westley, Edna V. Berger
`Lawrence C. Keary
`Index Editor: Jeffrey Schaefer
`Jeffrey M. Keller
`Art Associate: Joan K .. Akerlind
`P. Anthony Pinsonalilt
`Director of Corporate Communications: Gregory J. Thomas
`Anthony Sorce
`Electronic Publishing Coordinator: Joanne M. Pearson
`Trade Sales Manager: Robin B. Bartlett
`Electronic Publishing Designer: Kevin J. Leckner
`Trade Sales Account Executive: Bill Gaffney
`Direct Marketing Manager: ·Robert w. Chapman
`Art Director: Richard A. Weinstock
`Digital Photography: Shawn W. Cahill, Frank J. McElroy, Ill
`Marketing Communications Manager: Maryann Malorgio
`Director, Circulation & Fulfillment: Marianne Clarke
`Director, Professional Support Services: Mukesh Mehta, RPh
`Product Fulfillment Manager: Stephen Schweikhart
`Drug lnformaUon Specialists: Thomas Fleming, RPh, Marion Gray, RPh
`Editor, Special Projects: David w. Sitton
`
`~ Copyright © 1996 and published by Medical Economics Company at Montvale, Nj 07645-17 42. All rights reserved . None of the content of this public&
`•
`•
`tion may be reproduced, stored in a retrieval system, resold, redistributed, or transmitted in any form or by any means (electronic, mechanical , photo-
`copying, recotding, or otherwise) without the prior written permission of the publisher. PHYSICIANS' DESK REFERENCE®, PDR®, PDR For Nonprescription
`Drugs®, PDR For Ophthalmology®, Pocket PDR®, and The PDR® Family Guide to Prescription Drugs® are registered trademarks used herein under license. PDR®
`GenericsrM, PDR Guid;e to Drug lnteractions•Side Effects•lndications™, The PDR® Family Guide to Women's Health and Prescription DrugsrM, The PDR® Family
`Guide to Nutrition and Health'M, PDR® Electronic LibrarY'M, PDR® Drug Interactions, Side Effects, Indications Diskettes'M, and PDR® Drug REAX'M are trademarks
`used herein under license.
`
`Officers of Medical Economics: President and Chief Executive Officer: Norman R. Snesil ; President and Chief Operating Officer: Curtis B. Allen; Executive Vice
`President and Chief Financial Officer: J. Crispin Ashworth; Senior Vice President-Corporate Operations: John R. Ware; Senior VIce President-Corporate Business
`Development: Raymol'ld M. Zoeller; Vice President, Information Services and Chief Information Officer: Edward J. Zecchini
`
`ISBNs: 1-56363-152.() and 1·56363-156-3
`
`Metrics EX1042, Page 1
`
`

`
`OTC
`
`white, crystalline, water-soluble powder with a molecular
`weight of 553.91. The chemical structure is·presented below:
`Structural Formula:
`
`0
`
`~
`
`J ~ J
`
`CH20H
`NH -b-cH OH
`2 I
`2
`CH
`2QH
`
`2
`
`0-C-C-NH*NH-C- C-OH
`a
`!I
`!I
`!I
`I!
`00
`00
`
`~
`
`trome(cid:173)
`
`SUPERSALMON OIL 1000
`11000 mg.·Fresh Salmon Oill
`
`HOW SUPPLIED
`
`kplr Stfmon Oil 1000
`
`UlTAAGUARD
`iltlflh Potency Antoxidantl
`
`SIZE
`100's
`
`NDC#
`1088S.4001-5
`
`OTC
`
`i1iJt SUPPLIED
`
`'UitrtGuard
`
`SIZE
`60's
`
`NDC#
`1 088S.0720-3
`
`ULTRA VIM®
`!Antioxidant Multivitaminl
`
`ROll' SUPPLIED
`
`UltrtVim®
`
`OTC
`
`SIZE
`60's
`
`NDC#
`1088S.5313-3
`
`XL·1
`(Mu~ivitamin liquid with Mineralsl
`
`OTC
`
`HOW SUPPLIED
`
`SIZE
`8 oz.
`
`NDC#
`10888-8710-1
`
`Akorn, Inc.
`100 AKORN DRIVE
`ABITA SPRINGS, LA 70420
`
`Direct Inquiries to:
`(';ustomer Service
`. !8001 535-7155
`\004) 893-9300
`
`OPHTHALMIC PRODUCTS
`
`For information on Akorn ophthalmic pharmaceutical prod·
`ucts. consult the PDR For Ophthalmology. For literature,
`111mple material or service items, please contact Akorn, Inc.
`directly. (800) 535-7155
`
`Alcon Laboratories, Inc.
`and its affiliates
`CORPORATE HEADQUARTERS
`PO BOX 6600
`6201 SOUTH FREEWAY
`FORT WORTH, TX 76134
`
`Direct Inquiries to:
`Sales Services
`i8l71 293.0450
`For Medical Information Contact:
`Medical Department
`PO. Box 6380
`Fort Worth, TX 76115
`18171 293-0~50
`
`OPHTHALMIC PRODUCTS
`
`For information on Alcon ophthalmic products, consult the
`PDR For Ophthalmology. See a complete listing of products
`in the Manufacturers' Index section of this book. For infor(cid:173)
`mation, literature, samples or service items contact Alcon
`Sales Services.
`
`ALOMIDE® 0.1%
`ilodoxamide Tromethamine Ophthalmic Solutionl
`
`ij.
`
`D~IPTION
`AWMlDE® is a sterile ophthalmic solution containing the
`lllBSt cell stabilizer lodoxamide tromethamine for topical'
`admin~tration to the eyas. Lodoxamide tromethamine is a
`
`PRODUCT INFORMATION/469
`
`drugs are excreted in human milk, caution should be exer- ·
`cised when ALOMIDE® Ophthalmic Solution 0.1% is ad(cid:173)
`ministered to nursing women.
`Pediatric Use: Safety and effectiveness in pediatric patients
`below the age of 2 have not been established.
`ADVERSE REACTIONS
`During clin(cal studies of ALOMIDE® Ophthalmic Solution
`0.1 %, the most frequently reported ocular adverse experi(cid:173)
`ences were transient burning, stinging, or discomfort upon
`instillation, which occurred in approximately 15% of the
`subjects. Other ocular events occurring in 1 to 5% of the sub(cid:173)
`jects included ocular itching/pruritus, blurred vision, dry .
`eye, tearing/discharge, hyperemia, crystalline deposits, and
`foreign body sensation. Events that occurred in less than 1%
`of the subjects included corneal erosion/ulcer, scales on lid/
`lash, eye pain, ocular edema/swelling, ocular warming sen(cid:173)
`sation, ocular fatigue, chemosis, corneal abrasion, anterior
`chamber cells, keratopathy/keratitis, blepharitis, allergy,
`sticky sensation, and epitheliopathy.
`Nonocular events reported were he11dache (1.5%) and (at less
`than 1 %) heat sensation, dizziness, somnolence, nausea,
`stomach discomfort, sneezing, dry nose, and rash.
`OVERDOSAGE
`There have been no reports of ALOMIDE@ 0.1% (Lodoxa(cid:173)
`mide Tromethamine Ophthalmic Solution) overdOI!e follow(cid:173)
`ing topical ocular application. Accidental overdose of ail oral
`preparation of 120 to 180 mg oflodoxamide resulted in a tem(cid:173)
`porary sensation of warmth, profuse sweating, diarrhea,
`light-headedness, and a feeling of stomach distension; no'
`permanent adverse effects were observed. Side effects re(cid:173)
`ported following systemic oral administration of 0.1 mg to
`10.0 mg of lodoxamide include a feeling of warmth or flilsh·
`ing, headache, dizziness, fatigue, sweating, nausea, loose
`stools, and urinary frequency/urgency. The physician may
`consider emesis in the event of accidental ingestion.
`DOSAGE AND ADMINISTRATION
`The dose for adults imd children greater than two years of
`age is one to two drops in each affected eye four times daily ·
`for up to 3 months.
`HOW SUPPLJED
`ALOMIDE® Ophthalmic Solution 0.1% is supplied as
`follows: 10 mL in plastic ophthalmic DROP-TAINER@
`dispenser.
`
`10 mL: NDC 0065-0345-10
`
`STORAGE
`Sture at 15'C-27'C (59'F -SO'F).
`CAUTION
`Federal (USA>' law prohibits 'dispensing without prescrip(cid:173)
`tion.
`
`BETOPTIC®
`(betaxolol hydrochloride!
`0.5% as base
`Sterile Ophthalmic Solution
`
`DESCRIPTION
`BETOPTIC® Sterile Ophthalmic Solution contains betait·
`olol hydrochloride, a cardioselective beta-adrenergk recep(cid:173)
`tor blocking agent, in a sterile isotonic solution. Betaxolol
`hydrochloride is a white, crystalline powder, soluble iii wa(cid:173)
`ter, with •a molecular weight of 343.89. The chemical struc(cid:173)
`ture is presented below:
`
`Empirical Formula:
`C1sH28NOa · HCl
`Chemical Name:
`(±l-1-[p-[2-(Cyclopropylmethoxy)ethyl)phenoxy)-3-(iso(cid:173)
`propylaminol-2-propanol hydrochloride.
`Each mL of BETOPTIC Ophthalmic Solution (0.5%) con(cid:173)
`tains: Active: 5.6 mg betaxolol hydrochloride equivalent to
`betaxolol base 5 mg. Preservative: Benzalkonium Chloride
`O.Ql %. Inactives: Edetate Disodium, Sodium Chloride, Hy(cid:173)
`drochloric Acid and/ or Sodium Hydroxide (to adjust pH),
`and Purified Water.
`CUNICAL PHARMACOLOGY
`Betilxolol.HCl, a cardioselective (beta-1-adrenergic) receptor
`blocking agent, does not have significant membrane-stabiliz(cid:173)
`ing (local anesthetic) activity and is· devoid of intrinsic
`sympathomimetic action. Orally administered beta-adrener(cid:173)
`gic blocking agomts reduce cardiac output in healthy subjects
`and patients with heart disease. In patients with severe im(cid:173)
`pairment of myocardial function, beta-adrenergic receptor
`antagonists may inhibit the sympathetic stimulatory effect
`necessary to maintain adequate cardiac function.
`
`Continued on next page
`
`Consult 1996 supplements and future .editions fo~ revisions
`
`Chemical Name:
`N,N'-(2-chloro-5-cyano-m-phenylene)dioxamic acid
`thamine salt
`Empirical Formula: C1gli28012N5Cl
`Each ml of ALOMIDE@ Ophthalmic Solution contains: Ac··
`tive: 1.78 mg lodoxamide tromethamine equivalent to 1 mg
`lodoxamide. Preservative: benzalkonium chloride 0.007%.
`Inactive: mannitol, hydroxy'propyl methylcellulose 2910,
`sodium citrate, citric acid, edetate disodium, tyloxapol, hy·
`drochloric acid and/or sodium hydroxide (adjust pHI, and
`purified water.
`CUNICAL PHARMACOLOGY
`Lodoxamide tromethamine is a mast .cell stabilizer that
`inhibits the in vivo Type 1 immediate hypersensitivity
`reaction. Lodoxamide therapy inhibits the increases in cuta(cid:173)
`neous vascular permeability that are associated with reagin
`or IgE and antigen-mediated reactions.
`In vitro studies have demonstrated the ability of lodoxamide
`to stabilize rodent mast cells and prevent antigen-stimulated
`release of histamine. In addition, lodoxamide prevents the
`release of other mast cell inflammatory mediators (i.e., SRS(cid:173)
`A, slow-reacting substances of anaphylaxis, also known as
`the peptidoleukotrienes) and inhibits eosinophil chemotaxis.
`Although lodoxamide's precise mechanism of action is un(cid:173)
`known, the drug has been reported to prevent calcium influx
`into mast cells upon antigen stimulation.
`Lodoxamide has no intrinsic vasoconstrictor, antihistaminic,
`cyclooxygenase inhibition, or other anti-inflammatory activ(cid:173)
`ity.
`The disposition of 14C-lodoxamide was studied in six healthy
`adult volunteers receiving a 3 mg (50 ,...ci) oral dose of lodoxa(cid:173)
`mide. Urinary excretion was the major route of elimination.
`The elimination half-life of 1"C-lodoxamide.was 8.5 hours in
`urine. In a study conducted in twelve healthy adult volun(cid:173)
`teers, topical administration of ALOMIDE® 0.1% (Lqdoxa(cid:173)
`mide Tromethamine Ophthalmic Solution), one drop in each
`eye four times per day for ten days, did not result in any mea(cid:173)
`surable lodoxamide plasma levels at a detection limit of
`2.5 ng/mL.
`INDICATIONS AND USAGE
`ALOMIDE® Ophthalmic Solution 0.1% is indicated in the
`treatment of the ocular disorders referred to by the terms
`vernal keratoconjunctivitis, vernal conjunctivitis, and
`vernal keratitis.
`CONTRAINDICATIONS
`Hypersensitivity to any component of this product.
`WARNINGS
`Not for injection. As with all ophthalmic preparations
`containing benzalkonium chloride, patients should be in·
`structed not to wear soft contact lenses during treatment
`with ALOMIDE@ Ophthalmic Solution.
`PRECAUTIONS
`General: Patients inay experience a transient burning or
`stinging upon instillation of ALOMIDE® Ophthalmic Solu·
`tion. Should these symptOms persist, the patient should be
`advised to contact the prescribing physician.
`Carcinogenesis, Mutagenesis, Impairment of Fertility:
`.
`A long-term study with lodoxamide tromethamine in rats
`(two-year oral administration) showed no neoplastic or tu(cid:173)
`morigenic effects at do8es 100 mg/ kg/day (more than 5000
`times the proposed human clinical dose). No evidence of mu(cid:173)
`tagenicity or genetic damage was seen in the Ames Salmo(cid:173)
`nella Assay, Chrom<isomal Aberration in CHO Cells Assay,
`or Mouse Forward Lymphoma Assay. In the BALB/c-3T3
`Cells Transformation Assay, some increase in the number of
`transformed foci was seen at high concentrations (greater
`than 4000 p.g/mL). No evidence of impairment of reproduc(cid:173)
`tive function was shown in laboratory animal studies.
`P gnancy: Pregnancy Category B. Reproduction studies
`with lodoxamide tromethamine administered orally to rats
`and rabbits in doses oflOO mg/kg/day (more than 5000 times
`the proposed human clinical dose) produced no evidence of
`developmental toxicity. There are, however, no adequate
`and well-controlled studies in pregnant women. Because
`animal reproduction studies are not always predictive of
`human response, ALOMIDE® 0.1% (Lodoxamide Trome(cid:173)
`thamine Ophthalmic Solution) should be used during preg(cid:173)
`nancy only if clearly needed.
`Nursing Mothers: It is not known whether loooxamide
`
`tromethamine is excreted in human milk. Because many ---
`
`Metrics EX1042, Page 2